The present invention relates to a contraceptive and menstrual cycle controlling drug having oncostatic, antikinetosic preventive and therapeutic properties for treating mammary tumors and melanomas and a method therefor.
After several years of studies and experiments, related to the mechanism of action of melatonin, this indole is at present considered as the most important hormonal product of the pineal gland.
The developments in the field of receptor research have led to the localization of two important receptor sites of melatonin in SNC: the median eminence, pars tuberalis of the pituitary gland, and the supra chiasmatic nuclei of the hypothalamus.
Intensive studies have shown the biological basis for the mechanism of action of melatonin and its two halogen-derivatives (2-bromo and 2-iodomelatonin).
Experiments carried out by several researcher groups have confirmed some of the previous discoveries, and have shown that the ability of melatonin to inhibit reproduction, under given experimental conditions, can be related to a direct action of the indole on the hormone responsive elements in the SNC and the pituitary gland.
Thus, from prior research it has been known that melatonin can potentially be used as human contraceptive drug.
In fact, recently performed research has shown the possibility of using melatonin in association with a progestin compound (norethisterone), as a powerful contraceptive, which, moreover, provides several advantages such as: a low conception risk (less than 1%), lower risk of vascular disturbances (no estrogenic compounds are used) and less painful premenstrual and menstrual periods as well as a less painful pre-menopause period (melatonin and agonists thereof are known to have sedative effects).
Norethisterone alone, as well as other progestin derivatives, have been used as contraceptives in the recent years, and they are generally known under the name "mini-pill".
Norethisterone, when used as a "mini-pill", however has not provided remarkable results in preventing undesired pregnancies (about 2.35%).
Other progestinic compounds, such as 1-norgestrel, have been found to provide better results, with reduced doses (0.08-0.16 mg).
On the other hand, it has been found that melatonin, in order to express its contraceptive action. required comparatively high doses (100-200 mg).